Pharmacokinetics of sulphadimidine in Indian cattle calves (original) (raw)
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Pharmacokinetics and urinary excretion of sulphadimidine in sheep and goats
Journal of Veterinary Pharmacology and Therapeutics, 1979
Pharmacokinetics and urinary excretion of sulphadimidine were determined in sheep and goats following a single intravenous injection (100 mg/kg). The disposition of the drug was described in terms of exponential expression: Cp=Be-βt. Based on total (free and bound) sulphonamide level in plasma, pseudo-distribution equilibrium was rapidly attained and the half-life for elimination was 3.88 ± 0.64 h and 4.00 ± 0.34 h in sheep and goats, respectively. Body clearance, which is the sum of all clearance processes was 88 ± 19 and 55 ± 4 ml/kg/h in sheep and goats. Based on this study a satisfactory intravenous dosage regimen might consist of 100 and 60 mg sulphadimidine/kg body wt for sheep and goats and should be repeated at 12 h intervals. The influence of disease conditions on predicted plasma levels remain to be verified experimentally. Three-quarters of an intravenously injected dose of sulphadimidine was excreted in the urine of sheep and goats within 24 h of administration. The drug was mainly excreted as free amine while acetylated drug constituted 7 and 8% of total drug content in the urine of sheep and goats, respectively.
Disposition kinetics and dosage regimen of sulfadiadine in crossbred calves
Annales de recherches vétérinaires. Annals of veterinary research, 1990
After a single intravenous administration (100 mg/kg) of sulfadiadine to calves, the distribution half-life, elimination half-life and volume of distribution were 0.353 +/- 0.071 h, 11.2 +/- 0.79 h and 0.55 +/- 0.08 l/kg, respectively. Total body clearance and tissue/plasma ratio were calculated to be 34.8 +/- 4.6 ml.kg-1.1-1 and 1.34 +/- 0.38, respectively. A satisfactory intravenous dosage regimen of sulfadiadine in the treatment of infections in calves would be 125 mg/kg, followed by 100 mg/kg at 24 h intervals.
GSC Biological and Pharmaceutical Sciences, 2019
Due to the low cost and effectiveness of sulphadimidine against a wide variety of animal diseases, it is still being widely used in veterinary medicine. The present study was carried out to determine the effect of age on the pharmacokinetics of sulphadimidine in West African Dwarf (WAD) goats following intramuscular route of administration. Eight (8) WAD goats separated into two groups of four animals consisting of two males and two female goats each were used. Sulphadimdine sodium was administered at a dose of 100 mg/kg body weight. The goats in group one (3 months of age) and goats in group two (2 years old) were administered the drug on the right gluteal muscle. The pharmacokinetic parameters in the 3 months old WAD goats such as the maximum concentration (Cmax) (88.52±6.07), elimination half life (T1/2β) (3.79±0.29 h), volume of distribution (Vd) (4.55±0.46 L/kg), total body clearance (Cl) (0.77±0.09 L/kg/h) and mean residence time (MRT) (4.57 ± 0.48 h), were significantly (p<0.05) lower in comparison with Cmax (103. 59 ±7.56), T1/2β (4.90 h), Vd (13.03±1.58 L/kg), Cl (1.91±0.26 L/kg/h) and MRT (7.10±0.73 h) of the 2 years old WAD goats. The pharmacokinetic parameters of sulphadimidine in the 3 months old WAD goats were significantly different from that of the 2 years old WAD goats. This may be due to the difference in their body fat and water content.
Pharmacokinetic/Pharmacodinamics Integration of Sulfametazine in buffalo and cattle
Italian Journal of Animal Science, 2010
Sulfamethazine is a sulfonamide that presents a broad spectrum of activity, including Gram-positive and Gram-negative bacteria, Chlamydia spp. and some protozoa and it commonly used in ruminants. The aim of our work was to study the possible inter-species differences in the pharmacokinetic behavior and pharmacokinetic/ pharmacodynamic(PK/PD) integration of sulfamethazine after intravenous administration in buffalo and bovine. A single intravenous dose of 60 mg/kg was administered to six bovine and five buffalo (3-4 month old and weighting 120±15kg). Plasma concentrations of sulfamethazine were determined by high performance liquid chromatography. Differences between bovine and buffalo calves were found in t ½λ (buffaloes: t 1/2λ =6.17±0.58h; bovine t 1/2λ =7.46±1.05h), Cl (buffaloes: 45.31ml/h·kg; bovines 30.34ml/h·kg). As a consequence of the lower clearance in bovines, the AUC and t ½λ values were higher in this species. Important differences between bovine and buffalo exist for microorganisms that have a MIC value<32µg/ml related to time over minimum inhibitory concentration and weighted AUC.
The oral pharmacokinetics of three sulfonamides, sulfadimidine (pKa 7.5), sulfadiazine (pKa 6.5) and sulfanilamide (pKa 10.5), with different rates of unionization in rumen juice, were compared in Shiba goats to clarify the relationship between drug absorption profiles after their oral administration as well as their degree of unionization in the rumen. Sulfonamides were administered either into the left jugular vein or orally to five male goats at doses of 10 mg/kg body weight, using a crossover design with at least a 3-week washout period. The T max of sulfadimidine, sulfadiazine and sulfanilamide reached 2.0 ± 1.2, 6.0 ± 0.0, and 7.8 ± 1.6 hr, respectively, after their oral administration, and this was followed by their slow elimination due to a slow rate of drug absorption from the gastrointestinal tract. The MAT and t 1/2ka of sulfadiazine (13.2 ± 2.0 and 10.9 ± 1.08 hr) were significantly longer than those of sulfanilamide (9.09 ± 1.67 and 7.46 ± 1.70 hr) and sulfadimidine (7.52 ± 0.85 and 5.17 ± 0.66 hr). These results suggest that the absorption rates of highly unionized drugs (such as sulfanilamide and sulfadimidine) from the forestomach of goats may be markedly higher than less unionized ones (such as sulfadiazine). The mean oral bioavailability of sulfadiazine was high (83.9 ± 17.0%), whereas those of sulfadimidine and sulfanilamide were low (44.9 ± 16.4% and 49.2 ± 2.11%, respectively).
Some pharmacokinetic aspects of sulphadoxine alone and sulphadoxine-trimethoprim (TMP) combination were studied in goats following single intravenous (i.v) and intramuscular (i.m) administration of 15 mg kg-1 b.wt. After i.v injection the serum sulphadoxine concentration time course was best described by two compartment-open model with distribution half-lives (t0.5(α)) 2.48 and 2.31 h., elimination (t0.5(β)) half-lives 23.10 and 24.75 h., total body clearance (ClB) 0.076 and 0.073 L kg-1 h.-1 and steady state volume of distribution (Vdss) 368.54 and 411.73 ml kg-1 for sulphadoxine alone and sulphadoxine-trimethoprim combination, respectively. After i.m administration the mean peak serum concentrations (Cmax) 25.69 and 33.31 ug ml-1 were achieved after maximum time (tmax) of 3.09 and 2.79 h. for sulphadoxine alone and sulphadoxine-trimethoprim combination, respectively. The absorption half-lives (t0.5(ab)) were 0.58 and 0.42 h., respectively. It is concluded that a combination of sulphadoxine and TMP can provide a synergistic level for both antimicrobials and thus be a useful combination in the treatment of various goat diseases.
Pharmacokinetics of sulphadimidine in normal and febrile dogs
Journal of Veterinary Pharmacology and Therapeutics, 1982
Pharmacokinetic parameters which describe the distribution and elimination of sulphadimidine were determined in normal dogs and dogs in which fewer was produced by an intravenous injection of escherichia and staphylococcal species of bacteria. Sulphadimidine was injected as a single intravenous bolus at the dose of 100 mg/kg and the kinetics of the drug were described in terms of the biexponential expression: Cp = Ae-alpha t + Be-beta t. The distribution half-times of the drug were 1.52 h in the normal and 0.81 h in the febrile dogs. The drug distribution was significantly more rapid (P less than 0.05) in febrile than in normal dogs. Average +/- SD values for the half-lives of the drug were 16.2 +/- 5.7 h in normal and 16.7 +/- 4.7 h in the febrile dogs. The apparent volume of distribution (V&amp;amp;amp;amp;amp;#39;d(area)) was 628 +/- 251 ml/kg in the normal dogs, and was not statistically different from 495 +/- 144 ml/kg in the febrile dogs. The volume of the central compartment (V&amp;amp;amp;amp;amp;#39;c) was 445 +/- 55 ml/kg in normal dogs and this was significantly higher (P less than 0.01) than the V&amp;amp;amp;amp;amp;#39;c of 246 +/- 72 ml/kg in the febrile dogs. The body clearance was 22.4 +/- 4.8 and 20.2 +/- 3.6 ml/hour . kg in the normal and febrile dogs, respectively. The investigation revealed that the dosage regimen of sulphadimidine did not differ significantly between normal and febrile dogs.